Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion.

abstract：INTRODUCTION:Gestational diabetes mellitus (GDM) complicates 10% of all pregnancies and is defined as hyperglycemia first noted during pregnancy. Rates of GDM are rising and untreated GDM results in complications for both mother and fetus. GDM is often managed by diet and exercise but 30-40% of women will require pharm...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Malek R,Davis SN

更新日期：2016-06-01 00:00:00

abstract：:It has increasingly been recognized that few molecules move across the cell membrane without the assistance of transporter proteins. Large superfamilies of transporter proteins have been identified in every living cell, including microorganisms and mitochondria. This report reviews the role of transporters in physiolo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Lee EJ,Lean CB,Limenta LM

更新日期：2009-11-01 00:00:00

abstract：INTRODUCTION:Telaprevir is one of the first direct-acting antiviral drugs approved for the treatment of the hepatitis C virus (HCV) genotype 1. Following its approval in 2011, new data regarding the pharmacokinetics and pharmacodynamics were reported, leading to important clinical applications. AREAS COVERED:This arti...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Rivero-Juarez A,Camacho A,Rivero A

更新日期：2015-07-01 00:00:00

abstract：INTRODUCTION:The second-line treatment of endometriosis-related pain symptoms includes injectable depot formulations of gonadotropin-releasing hormone analogs (GnRH-as). These drugs improve the symptomatology by inducing a hypoestrogenic status and a consequent regression of endometriotic implants. However, GnRH-a may ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Della Corte L,Barra F,Mercorio A,Evangelisti G,Rapisarda AMC,Ferrero S,Bifulco G,Giampaolino P

更新日期：2020-09-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Cytochrome (CYP) P450 is a collective name for a very large group of heme enzymes, which catalyze largely oxidative reactions, including those of pharmacological and toxicological importance. Their efficient operation requires coupling of specific electron donor and O(2) consumption and substrat...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Shakunthala N

更新日期：2010-01-01 00:00:00

abstract：:Luminogenic cytochrome P450 (CYP) assays couple CYP enzyme activity to firefly luciferase luminescence in a technology called P450-Glo(TM) (Promega). Luminogenic substrates are used in assays of human CYP1A1, -1A2, -1B1, -2C8, -2C9, -2C19, -2D6, -2J2, -3A4, -3A7, -4A11, -4F3B, -4F12 and -19. The assays detect dose-dep...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Cali JJ,Ma D,Sobol M,Simpson DJ,Frackman S,Good TD,Daily WJ,Liu D

更新日期：2006-08-01 00:00:00

abstract：:The in vitro pharmacological profiling of drugs using a large panel of cloned receptors (e.g., G protein-coupled receptors, ligand-gated ion channels, Na(+)-dependent monoamine transporters), an approach that has come to be known as 'receptorome screening', has unveiled novel molecular mechanisms responsible for the a...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Setola V,Roth BL

更新日期：2005-10-01 00:00:00

abstract：:Toxicogenomics is the application of gene expression profiling technology to toxicology. This results in the generation of very large and complex gene expression data sets associated with the development of toxicities. It is widely assumed that this data can be deconvoluted to reveal novel insights into toxicological ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Huby R,Tugwood JD

更新日期：2005-08-01 00:00:00

abstract：INTRODUCTION:Replacement therapy for FVIII/IX in hemophilia A/B is more than 50 years old following the discovery of cryoprecipitate by Judith Pool in 1964. On-demand therapy and prophylaxis to treat or prevent bleedings is very demanding owing to the short half-life (HL) of factor concentrates (no more than 12-14 h fo...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Morfini M

更新日期：2016-11-01 00:00:00

abstract：INTRODUCTION:Oral mucositis, one of the major side effects of chemotherapy and irradiation, is still a burden of modern oncology. The keratinocyte growth factor (KGF) palifermin has been approved as a new, targeted therapy for the prevention of severe oral mucositis. AREAS COVERED:The authors review the literature on ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Weigelt C,Haas R,Kobbe G

更新日期：2011-04-01 00:00:00

abstract：INTRODUCTION:Sesamin is a major lignan found in sesame and is known to have various biological effects. Some of these biological effects occur following its metabolic conversion to corresponding catechols and, therefore, the study of sesamin metabolism is quite important. There is currently a need to identify the enzym...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Yasuda K,Sakaki T

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:The number of patients eligible for cardiovascular therapies in general is forecast to increase substantially in the coming decades. However, the current list of potential future cardiovascular blockbuster drugs is alarmingly short. There is thus a clear need for innovative strategies to increase the efficie...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Jänis MT,Laaksonen R,Oresic M

更新日期：2008-06-01 00:00:00

abstract：INTRODUCTION:Invasive fungal infections remain a leading cause of infectious morbidity and mortality in immunocompromised patients. There are relatively few effective antifungal agents, and currently available agents all have significant limitations. Isavuconazole is a novel second-generation triazole with broad-spectr...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Livermore J,Hope W

更新日期：2012-06-01 00:00:00

abstract：BACKGROUND:5-Aminosalicylate (5-ASA) agents are the mainstay of oral therapy for ulcerative colitis (UC). Balsalazide, a prodrug of 5-ASA, has recently been approved for the treatment of UC. OBJECTIVE:To summarize current data on balsalazide and to discuss its impact on management of UC. METHODS:A systematic review o...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Wiggins JB,Rajapakse R

更新日期：2009-10-01 00:00:00

abstract：INTRODUCTION:Type 2 diabetes often involves derangements in lipid levels in addition to insulin resistance and diminishing insulin secretion. Colesevelam hydrochloride, a bile acid sequestrant (BAS), is approved for adjunctive therapy to diet and exercise for glycemic control in type 2 diabetes. In clinical studies in ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Younk LM,Davis SN

更新日期：2012-04-01 00:00:00

abstract：INTRODUCTION:This meeting report presents a brief summary on the 4th Annual Predictive Toxicology Summit 2012, which was held on 15 - 16 February 2012 in London. AREAS COVERED:The majority of presentations came from global pharmaceutical companies, although small and medium enterprise (SME) and academic researchers we...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Cui Z

更新日期：2013-08-01 00:00:00

abstract：INTRODUCTION:In vitro genotoxicity assays have a high sensitivity to detect rodent carcinogens, but mammalian cell tests have a propensity for misleading positive results (poor specificity). Recent data show a greater risk of misleading positive results in p53-deficient rodent cell lines than in p53-competent human cel...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Kirkland D

更新日期：2011-12-01 00:00:00

abstract：INTRODUCTION:Assessments of the pharmacokinetic/pharmacodynamic (PK/PD) characteristics are an integral part in the development of novel therapeutic agents. Compared with traditional small molecule drugs, therapeutic proteins possess many distinct PK/PD features that necessitate the application of modified or separate ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Diao L,Meibohm B

更新日期：2015-07-01 00:00:00

abstract：INTRODUCTION:Omalizumab is a subcutaneously administrated monoclonal anti-IgE antibody indicated in adults, adolescents and children 6 years of age and older with moderate to severe allergic asthma uncontrolled by conventional pharmacological treatments and sensitization to at least one perennial allergen. Area covered...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Luu M,Bardou M,Bonniaud P,Goirand F

更新日期：2016-12-01 00:00:00

abstract：INTRODUCTION:Maintaining effective antiretroviral treatment for life is a major problem in both resource-limited and resource-rich countries. Despite the progress observed in paediatric antiretroviral therapy, approximately 12% of children still experience treatment failure due to drug resistance, inadequate dosing and...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Piana C,Danhof M,Della Pasqua O

更新日期：2017-05-01 00:00:00

abstract：:Acute kidney injury is a common condition and is associated with a high mortality rate. It has been recognised that routinely used measures of renal function, such as levels of blood urea nitrogen and serum creatinine, increase significantly only after substantial kidney injury occurs and then with a time delay. Insen...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Vaidya VS,Bonventre JV

更新日期：2006-10-01 00:00:00

abstract：:The pharmaceutical relevance of proton-coupled peptide transporters is currently under intense investigation in many laboratories. Studies have shown that these membrane proteins, expressed in intestine, kidney, choroid plexus and other tissues, accept many peptidomimetic drugs and prodrugs as substrates. The focus of...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Brandsch M

更新日期：2009-08-01 00:00:00

abstract：:Introduction: Antiepileptic drugs (AEDs) are the cornerstone of treatment of patients with epilepsy, and there are presently 27 licensed AEDs making AEDs among the most common medications for which therapeutic drug monitoring (TDM) is performed. The aim of this review is to provide an overview of the current evidence ...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Johannessen Landmark C,Johannessen SI,Patsalos PN

更新日期：2020-03-01 00:00:00

abstract：INTRODUCTION:A more concentrated insulin glargine formulation, containing 300 U/mL (Gla-300) was approved in 2015 in the US and Europe for the treatment of diabetes mellitus in adults. AREAS COVERED:This drug evaluation focuses on the pharmacokinetics (PK) and pharmacodynamics (PD) of Gla-300 from studies published up...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Owens DR

更新日期：2016-08-01 00:00:00

abstract：INTRODUCTION:The association between pregnancy and altered drug pharmacokinetic (PK) properties is acknowledged, as is its impact on drug plasma concentrations and thus therapeutic efficacy. However, there have been few robust PK studies of antimalarial use in pregnancy. Given that inadequate dosing for prevention or t...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Moore BR,Davis TM

更新日期：2020-09-01 00:00:00

abstract：INTRODUCTION:Mortality from invasive fungal disease involving the central nervous system (CNS) is excessive. Achieving therapeutic drug concentrations at the site of infection within the CNS is always difficult and its evaluation is complex due to anatomical barriers and variable pathophysiological lesions. Areas cover...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Stott KE,Hope W

更新日期：2018-08-01 00:00:00

abstract：:Several first-line antihypertensive drugs, including calcium channel blockers, beta-adrenergic blockers and angiotensin receptor blockers, undergo metabolism through different CYP isoforms. As a consequence of CYP-dependent metabolism, wide interindividual variability of plasma concentrations of antihypertensive drugs...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Höcht C,Bertera FM,Mayer MA,Taira CA

更新日期：2010-02-01 00:00:00

abstract：INTRODUCTION:Cardiovascular disease is still the leading cause of death worldwide. There are many environmental and genetic factors that play a role in the development of cardiovascular disease. The treatment of cardiovascular disease is beginning to move in the direction of personalized medicine by using biomarkers fr...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Berinstein E,Levy A

更新日期：2017-09-01 00:00:00

abstract：INTRODUCTION:Antiepileptic drugs (AEDs) are widely used for the treatment of epilepsy. However, ∼ 30% of patients do not remain seizure free. It is possible that methylxanthine derivatives (e.g., caffeine and theophylline) may partially account for this outcome. AREAS COVERED:Data on the convulsive activity of methylx...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Chrościńska-Krawczyk M,Radzik I,Miziak B,Czuczwar SJ

更新日期：2014-07-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:The prevalence of acute renal allograft rejection has decreased substantially in past decades due to new and more specific immunosuppressive compounds but improvements in long-term graft function have not been achieved. There is a large need for new immunosuppressive agents that lack toxicity of...

journal_title：Expert opinion on drug metabolism & toxicology

authors： Matz M,Naik M,Mashreghi MF,Glander P,Neumayer HH,Budde K

更新日期：2011-01-01 00:00:00